WO2018086585A8 - Nitrogen-containing heterocyclic compounds, preparation method therefor, pharmaceutical composition thereof, and applications thereof - Google Patents

Nitrogen-containing heterocyclic compounds, preparation method therefor, pharmaceutical composition thereof, and applications thereof Download PDF

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Publication number
WO2018086585A8
WO2018086585A8 PCT/CN2017/110438 CN2017110438W WO2018086585A8 WO 2018086585 A8 WO2018086585 A8 WO 2018086585A8 CN 2017110438 W CN2017110438 W CN 2017110438W WO 2018086585 A8 WO2018086585 A8 WO 2018086585A8
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WO
WIPO (PCT)
Prior art keywords
nitrogen
containing heterocyclic
heterocyclic compounds
applications
preparation
Prior art date
Application number
PCT/CN2017/110438
Other languages
French (fr)
Chinese (zh)
Other versions
WO2018086585A1 (en
Inventor
胡永韩
蔡冬梅
董平
朱久香
李曼华
董加强
王铁林
Original Assignee
山东罗欣药业集团股份有限公司
罗欣生物科技(上海)有限公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by 山东罗欣药业集团股份有限公司, 罗欣生物科技(上海)有限公司 filed Critical 山东罗欣药业集团股份有限公司
Priority to CN201780067789.4A priority Critical patent/CN110088101A/en
Publication of WO2018086585A1 publication Critical patent/WO2018086585A1/en
Publication of WO2018086585A8 publication Critical patent/WO2018086585A8/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/46Iso-indoles; Hydrogenated iso-indoles with an oxygen atom in position 1
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Disclosed in the present invention are nitrogen-containing heterocyclic compounds, a preparation method therefor, a pharmaceutical composition thereof, and applications thereof. The nitrogen-containing heterocyclic compounds represented by formula II can be effectively combined with bromodomains of BRD4, BRD3, BRD2 and BRDT of a BET family, and play a specific role.
PCT/CN2017/110438 2016-11-10 2017-11-10 Nitrogen-containing heterocyclic compounds, preparation method therefor, pharmaceutical composition thereof, and applications thereof WO2018086585A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201780067789.4A CN110088101A (en) 2016-11-10 2017-11-10 A kind of nitrogen-containing hetero cyclics, preparation method, pharmaceutical composition and application

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201610989839.1 2016-11-10
CN201610989839.1A CN108069959A (en) 2016-11-10 2016-11-10 A kind of nitrogen-containing hetero cyclics, its preparation method, pharmaceutical composition and application

Publications (2)

Publication Number Publication Date
WO2018086585A1 WO2018086585A1 (en) 2018-05-17
WO2018086585A8 true WO2018086585A8 (en) 2018-06-21

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PCT/CN2017/110438 WO2018086585A1 (en) 2016-11-10 2017-11-10 Nitrogen-containing heterocyclic compounds, preparation method therefor, pharmaceutical composition thereof, and applications thereof

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CN (2) CN108069959A (en)
WO (1) WO2018086585A1 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108794477A (en) * 2018-08-06 2018-11-13 华东师范大学 A kind of N2The preparation method of 9 substituted guanine class compound
TW202110818A (en) * 2019-05-24 2021-03-16 美商拜歐斯瑞克斯公司 Compounds targeting proteins and pharmaceutical compositions thereof, and their therapeutic applications
CN112079829B (en) * 2019-06-14 2021-11-26 四川大学 1,2, 4-triazole [4,3-a ] pyridine derivative and preparation method and application thereof
CN110183372B (en) * 2019-06-20 2020-10-30 山东大学 Isatin compound and preparation method and application thereof
CN110272418B (en) * 2019-07-25 2020-10-16 山东大学 Triazole compound and preparation method and application thereof
CN113754541A (en) * 2020-06-02 2021-12-07 深圳湾实验室 Micromolecule inhibitor targeting EB virus nuclear antigen protein, preparation method and application thereof
WO2022033542A1 (en) * 2020-08-14 2022-02-17 南京明德新药研发有限公司 5-membered heteroaromatic pyridone compounds and application thereof
CN112225741B (en) * 2020-12-09 2021-03-30 中山大学 Application of 1,2, 4-triazolo 4,3-B pyridazine derivative in preparation of anti-inflammatory factor storm medicines
CN115028646B (en) * 2022-05-31 2023-06-30 山东第一医科大学(山东省医学科学院) Nitrogen-containing heterocyclic compound, preparation method and application thereof in antitumor preparation
CN115557954B (en) * 2022-11-11 2024-06-11 上海泰坦科技股份有限公司 Preparation method of 6-bromo- [1,2,4] triazolo [4,3-b ] pyridazine

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2014012635A (en) * 2012-04-20 2015-05-15 Abbvie Inc Isoindolone derivatives.
CN105164127A (en) * 2013-03-11 2015-12-16 艾伯维公司 Bromodomain inhibitors
PL3290407T3 (en) * 2013-10-18 2020-09-07 Celgene Quanticel Research, Inc Bromodomain inhibitors
CN105254635A (en) * 2015-10-30 2016-01-20 中国药科大学 Imidazo pyrazine compound, medicine composition of imidazo pyrazine compound and purpose of imidazo pyrazine compound

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WO2018086585A1 (en) 2018-05-17
CN108069959A (en) 2018-05-25
CN110088101A (en) 2019-08-02

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